UCB-9260 是口服活性小分子,通过稳定三聚体的不对称形式抑制肿瘤坏死因子信号传导。它对肿瘤坏死因子的选择性高于其他超家族成员,并与肿瘤坏死因子结合,其Kd值为 13?nM。
产品描述
UCB-9260 inhibits TNF signaling by stabilizing an asymmetric form of the trimer.
体外活性
In Hek-293 cells, UCB-9260 (0-10 μM)?inhibits NF-κB with a geometric mean IC50?of 202?nM after TNF (10?pM) stimulation. UCB-9260?inhibits TNF-dependent cytotoxicity with a geometric mean IC50?of 116?nM and a geometric mean IC50?of 120?nM, using human and mouse TNF, respectively.
体内活性
UCB-9260 (150?mg/kg; p.o.) treatment twice daily?for 7 days shows a significant reduction of the clinical score. In adult male Balb/c mice, UCB-9260?(10-300?mg/kg; p.o.) dose-dependently inhibits human and mouse TNF-induced neutrophil recruitment to the peritoneal compartment.
Cas No.
1515888-53-5
分子式
C26H25N5O
分子量
423.51
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years